+441518081136Understanding the pharmacology and toxicology properties of transdermal Buprenorphine and Fentanyl to ensure the safety and efficacy of drugs use
7th World Congress on Clinical Pharmacy and Pharmacy Practice
December 07-09, 2017 | Rome, Italy
Christina Yuen Ki Leung
The University of Hong Kong, China
Scientific Tracks Abstracts : J Pharmacol Ther Res
Abstract:
Buprenorphine and Fentanyl transdermal patches are used for the management of chronic intractable pain in both malignant and nonmalignant patients. Both Buprenorphine and Fentanyl are potent opioids, but they have different pharmacology and toxicology properties. It is important to understand the difference in these properties as this information is useful for clinicians and pharmacists to use the opioid patches safely and effectively. Opioid analgesics mimic endogenous opioid peptides by causing a prolonged activation of opioid receptors (usually μ receptor). This receptor medicates analgesia, respiratory depression, euphoria and sedation. Fentanyl is potent, highly lipid soluble, rapidly acting μ-opioid receptor full agonist. Buprenorphine is a highly lipophilic semisynthetic opioid. It has complex pharmacology which is different from Fentanyl. Buprenorphine is a partial μ-opioid receptor agonist which binds to and activates a receptor, but has only partial efficacy compared to a full agonist. This means that it may have ceiling effect and demonstrate both agonist and antagonist effects. In human studies using clinical effective analgesia doses, Buprenorphine does not have a ceiling effect to analgesia. However, Buprenorphine does have a ceiling effect for respiratory depression. Hence, higher doses can be given with fewer respiratory depression side effect compared with higher doses of Fentanyl. The primary side effects of Buprenorphine are similar to Fentanyl (eg, nausea, vomiting, and constipation), but the intensity of these side effects is reduced significantly compared to full agonist, Fentanyl. The most severe and serious adverse reaction associated with opioid use is respiratory depression, the mechanism is behind fatal overdose. Buprenorphine behaves differently than Fentanyl in this respect, as it shows a ceiling effect for respiratory depression. Buprenorphine has slowed off rate (half-life of association/dissociation is 2–5 hours). The slow dissociation from μ-receptor accounts for its prolonged therapeutic effect for treatment of pain. Respiratory depression is rare with buprenorphine, but If occurs, it can be reversed by Naloxone, often larger doses are required than Fentanyl because Buprenorphine dissociates slowly from the receptors. In conclusions, the pharmacology profile of Buprenorphine is complex but unique, and contributes to its distinct safety and efficacy when it is used under appropriate clinical indications.
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